Discovery of N-(4-(3-isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-4-(4-methylpiperazin-1-yl)quinazolin-7-amine as a Novel, Potent, and Oral Cyclin-Dependent Kinase Inhibitor against Haematological Malignancies was written by Huang, Jianhang;Wang, Xinren;Dong, Ruinan;Liu, Xiaoyue;Li, Hongmei;Zhang, Tianyi;Xu, Junyu;Liu, Chenhe;Zhang, Yanmin;Hou, Shaohua;Tang, Weifang;Lu, Tao;Chen, Yadong. And the article was included in Journal of Medicinal Chemistry in 2021.Synthetic Route of C3H9NO The following contents are mentioned in the article:
Hematol. malignancies (HM) start in blood forming tissue or in the cells of the immune system. Cyclin-dependent kinases (CDKs) regulate cell cycle progression, and some of them control cellular transcription. CDK inhibition can trigger apoptosis and could be particularly useful in hematol. malignancies. Herein, we describe our efforts toward the discovery of a novel series of quinazoline derivatives as CDK inhibitors. Intensive structural modifications lead to the identification of compound 37d as the most active inhibitors of CDKs 1, 2, 4, 8 and 9 with balancing potency and selectivity against CDKs. Further biol. studies revealed that compound 37d can arrest the cell cycle and induce apoptosis via activating PARP and caspase 3. More importantly, compound 37d showed good antitumor efficacy in multiple HM mice xenograft models with no obvious toxicity. These results indicated that CDK 1, 2, 4, 8, and 9 inhibitors could be potentially used to treat certain hematol. malignancies. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Synthetic Route of C3H9NO).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Synthetic Route of C3H9NO
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem